ES2668351T3 - Nuevos polimorfos y nuevos estados sólidos de tiacumicina B - Google Patents

Nuevos polimorfos y nuevos estados sólidos de tiacumicina B Download PDF

Info

Publication number: ES2668351T3
Authority: ES; Spain
Prior art keywords: thiacumycin; crystalline; solvate; xrpd; new
Prior art date: 2014-03-18
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.): Active

Application number

ES15711122.0T

Other languages

English (en)

Spanish (es)

Inventor

Stefan Kluge

Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)

Xellia Pharmaceuticals ApS

Original Assignee

Xellia Pharmaceuticals ApS

Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)

2014-03-18

Filing date

2015-03-17

Publication date

2018-05-17

2015-03-17 Application filed by Xellia Pharmaceuticals ApS filed Critical Xellia Pharmaceuticals ApS

2018-05-17 Application granted granted Critical

2018-05-17 Publication of ES2668351T3 publication Critical patent/ES2668351T3/es

Status Active legal-status Critical Current

2035-03-17 Anticipated expiration legal-status Critical

Links

239000007787 solid Substances 0.000 title description 26
239000012453 solvate Substances 0.000 claims abstract description 97
QTBSBXVTEAMEQO-UHFFFAOYSA-N Acetic acid Chemical compound CC(O)=O QTBSBXVTEAMEQO-UHFFFAOYSA-N 0.000 claims abstract description 57
JMMWKPVZQRWMSS-UHFFFAOYSA-N isopropanol acetate Natural products CC(C)OC(C)=O JMMWKPVZQRWMSS-UHFFFAOYSA-N 0.000 claims abstract description 9
229940011051 isopropyl acetate Drugs 0.000 claims abstract description 9
GWYFCOCPABKNJV-UHFFFAOYSA-N isovaleric acid Chemical compound CC(C)CC(O)=O GWYFCOCPABKNJV-UHFFFAOYSA-N 0.000 claims abstract description 9
238000000634 powder X-ray diffraction Methods 0.000 claims description 62
239000000463 material Substances 0.000 description 34
ZWEHNKRNPOVVGH-UHFFFAOYSA-N 2-Butanone Chemical compound CCC(C)=O ZWEHNKRNPOVVGH-UHFFFAOYSA-N 0.000 description 28
239000013078 crystal Substances 0.000 description 25
KFZMGEQAYNKOFK-UHFFFAOYSA-N Isopropanol Chemical compound CC(C)O KFZMGEQAYNKOFK-UHFFFAOYSA-N 0.000 description 24
238000003860 storage Methods 0.000 description 20
MVPPADPHJFYWMZ-UHFFFAOYSA-N chlorobenzene Chemical compound ClC1=CC=CC=C1 MVPPADPHJFYWMZ-UHFFFAOYSA-N 0.000 description 18
BDERNNFJNOPAEC-UHFFFAOYSA-N propan-1-ol Chemical compound CCCO BDERNNFJNOPAEC-UHFFFAOYSA-N 0.000 description 18
239000002904 solvent Substances 0.000 description 18
XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 18
150000001875 compounds Chemical class 0.000 description 16
238000004128 high performance liquid chromatography Methods 0.000 description 10
IMNFDUFMRHMDMM-UHFFFAOYSA-N N-Heptane Chemical compound CCCCCCC IMNFDUFMRHMDMM-UHFFFAOYSA-N 0.000 description 9
229940032007 methylethyl ketone Drugs 0.000 description 9
238000000034 method Methods 0.000 description 8
239000000725 suspension Substances 0.000 description 8
239000007858 starting material Substances 0.000 description 7
238000000003 thermogravimetry coupled to Fourier transform infrared spectroscopy Methods 0.000 description 7
WEVYAHXRMPXWCK-UHFFFAOYSA-N Acetonitrile Chemical compound CC#N WEVYAHXRMPXWCK-UHFFFAOYSA-N 0.000 description 6
239000000243 solution Substances 0.000 description 6
239000003814 drug Substances 0.000 description 5
DTQVDTLACAAQTR-UHFFFAOYSA-N Trifluoroacetic acid Chemical compound OC(=O)C(F)(F)F DTQVDTLACAAQTR-UHFFFAOYSA-N 0.000 description 4
238000002425 crystallisation Methods 0.000 description 4
230000008025 crystallization Effects 0.000 description 4
229940079593 drug Drugs 0.000 description 4
239000012535 impurity Substances 0.000 description 4
239000002002 slurry Substances 0.000 description 4
QTBSBXVTEAMEQO-UHFFFAOYSA-M Acetate Chemical compound CC([O-])=O QTBSBXVTEAMEQO-UHFFFAOYSA-M 0.000 description 3
229960000074 biopharmaceutical Drugs 0.000 description 3
238000004090 dissolution Methods 0.000 description 3
239000011440 grout Substances 0.000 description 3
150000004677 hydrates Chemical class 0.000 description 3
238000005259 measurement Methods 0.000 description 3
239000000126 substance Substances 0.000 description 3
241000183229 Actinoplanes deccanensis Species 0.000 description 2
RYGMFSIKBFXOCR-UHFFFAOYSA-N Copper Chemical compound [Cu] RYGMFSIKBFXOCR-UHFFFAOYSA-N 0.000 description 2
241001495431 Dactylosporangium aurantiacum Species 0.000 description 2
238000010521 absorption reaction Methods 0.000 description 2
230000005540 biological transmission Effects 0.000 description 2
229910052802 copper Inorganic materials 0.000 description 2
239000010949 copper Substances 0.000 description 2
238000000855 fermentation Methods 0.000 description 2
230000004151 fermentation Effects 0.000 description 2
238000004108 freeze drying Methods 0.000 description 2
125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 description 2
238000002360 preparation method Methods 0.000 description 2
230000005855 radiation Effects 0.000 description 2
102100031480 Dual specificity mitogen-activated protein kinase kinase 1 Human genes 0.000 description 1
101710146526 Dual specificity mitogen-activated protein kinase kinase 1 Proteins 0.000 description 1
VYPSYNLAJGMNEJ-UHFFFAOYSA-N Silicium dioxide Chemical compound O=[Si]=O VYPSYNLAJGMNEJ-UHFFFAOYSA-N 0.000 description 1
238000002441 X-ray diffraction Methods 0.000 description 1
239000012296 anti-solvent Substances 0.000 description 1
230000009286 beneficial effect Effects 0.000 description 1
230000015572 biosynthetic process Effects 0.000 description 1
230000036765 blood level Effects 0.000 description 1
230000000052 comparative effect Effects 0.000 description 1
238000001816 cooling Methods 0.000 description 1
238000004807 desolvation Methods 0.000 description 1
238000001514 detection method Methods 0.000 description 1
239000002552 dosage form Substances 0.000 description 1
239000000428 dust Substances 0.000 description 1
230000000694 effects Effects 0.000 description 1
238000001914 filtration Methods 0.000 description 1
239000012847 fine chemical Substances 0.000 description 1
230000009477 glass transition Effects 0.000 description 1
230000012010 growth Effects 0.000 description 1
230000007773 growth pattern Effects 0.000 description 1
230000009931 harmful effect Effects 0.000 description 1
230000036571 hydration Effects 0.000 description 1
238000006703 hydration reaction Methods 0.000 description 1
229910052739 hydrogen Inorganic materials 0.000 description 1
239000001257 hydrogen Substances 0.000 description 1
125000004435 hydrogen atom Chemical group [H]* 0.000 description 1
238000002347 injection Methods 0.000 description 1
239000007924 injection Substances 0.000 description 1
230000003993 interaction Effects 0.000 description 1
230000007774 longterm Effects 0.000 description 1
238000004519 manufacturing process Methods 0.000 description 1
238000002844 melting Methods 0.000 description 1
230000008018 melting Effects 0.000 description 1
229910021421 monocrystalline silicon Inorganic materials 0.000 description 1
239000003960 organic solvent Substances 0.000 description 1
239000002245 particle Substances 0.000 description 1
239000000546 pharmaceutical excipient Substances 0.000 description 1
229940124531 pharmaceutical excipient Drugs 0.000 description 1
230000000144 pharmacologic effect Effects 0.000 description 1
230000000704 physical effect Effects 0.000 description 1
102000054765 polymorphisms of proteins Human genes 0.000 description 1
239000000843 powder Substances 0.000 description 1
239000012047 saturated solution Substances 0.000 description 1
238000012216 screening Methods 0.000 description 1
238000007614 solvation Methods 0.000 description 1
238000001694 spray drying Methods 0.000 description 1

Classifications

- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
- C07H17/00—Compounds containing heterocyclic radicals directly attached to hetero atoms of saccharide radicals
- C07H17/04—Heterocyclic radicals containing only oxygen as ring hetero atoms
- C07H17/08—Hetero rings containing eight or more ring members, e.g. erythromycins
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/70—Carbohydrates; Sugars; Derivatives thereof
- A61K31/7042—Compounds having saccharide radicals and heterocyclic rings
- A61K31/7048—Compounds having saccharide radicals and heterocyclic rings having oxygen as a ring hetero atom, e.g. leucoglucosan, hesperidin, erythromycin, nystatin, digitoxin or digoxin
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/04—Antibacterial agents
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
- C07B2200/00—Indexing scheme relating to specific properties of organic compounds
- C07B2200/13—Crystalline forms, e.g. polymorphs

Landscapes

Health & Medical Sciences (AREA)
Chemical & Material Sciences (AREA)
Organic Chemistry (AREA)
Life Sciences & Earth Sciences (AREA)
General Health & Medical Sciences (AREA)
Molecular Biology (AREA)
Pharmacology & Pharmacy (AREA)
Animal Behavior & Ethology (AREA)
Medicinal Chemistry (AREA)
Public Health (AREA)
Veterinary Medicine (AREA)
Engineering & Computer Science (AREA)
Biochemistry (AREA)
Biotechnology (AREA)
Genetics & Genomics (AREA)
Chemical Kinetics & Catalysis (AREA)
Communicable Diseases (AREA)
Oncology (AREA)
General Chemical & Material Sciences (AREA)
Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
Epidemiology (AREA)
Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
Saccharide Compounds (AREA)

ES15711122.0T 2014-03-18 2015-03-17 Nuevos polimorfos y nuevos estados sólidos de tiacumicina B Active ES2668351T3 (es)

Applications Claiming Priority (5)

Application Number	Priority Date	Filing Date	Title
US201461954715P	2014-03-18	2014-03-18
US201461954715P		2014-03-18
US201462020570P	2014-07-03	2014-07-03
US201462020570P		2014-07-03
PCT/EP2015/055531 WO2015140153A1 (fr)	2014-03-18	2015-03-17	Nouveaux polymorphes et nouveaux états solides de la tiacumicine b

Publications (1)

Publication Number	Publication Date
ES2668351T3 true ES2668351T3 (es)	2018-05-17

Family

ID=52697399

Family Applications (1)

Application Number	Title	Priority Date	Filing Date
ES15711122.0T Active ES2668351T3 (es)	2014-03-18	2015-03-17	Nuevos polimorfos y nuevos estados sólidos de tiacumicina B

Country Status (17)

Country	Link
US (1)	US10227371B2 (fr)
EP (1)	EP3119793B1 (fr)
JP (1)	JP2017507994A (fr)
KR (1)	KR20160134719A (fr)
CN (1)	CN106103462A (fr)
AU (1)	AU2015233583B2 (fr)
BR (1)	BR112016021542B1 (fr)
CA (1)	CA2940902C (fr)
DK (1)	DK3119793T3 (fr)
ES (1)	ES2668351T3 (fr)
HR (1)	HRP20180668T1 (fr)
HU (1)	HUE038426T2 (fr)
IL (2)	IL247726A0 (fr)
PL (1)	PL3119793T3 (fr)
PT (1)	PT3119793T (fr)
SI (1)	SI3119793T1 (fr)
WO (1)	WO2015140153A1 (fr)

Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number	Priority date	Publication date	Assignee	Title
CN108727387B (zh) *	2018-07-25	2021-03-16	天津大学	依鲁替尼乙酸异丙酯溶剂化合物及其制备方法
CN109053738B (zh) *	2018-08-29	2020-10-16	浙江工业大学	一种依鲁替尼的溶剂化物及其制备方法
CN114224899B (zh) *	2020-09-09	2024-04-26	首都医科大学附属北京胸科医院	非达霉素用于制备抑制脓肿分枝杆菌活性的产品

Family Cites Families (8)

* Cited by examiner, † Cited by third party
Publication number	Priority date	Publication date	Assignee	Title
US4918174A (en)	1986-09-26	1990-04-17	Abbott Laboratories	Tiacumicin compounds
WO2004014295A2 (fr)	2002-07-29	2004-02-19	Optimer Pharmaceuticals, Inc.	Fabrication de tiacumicine
US7378508B2 (en) *	2007-01-22	2008-05-27	Optimer Pharmaceuticals, Inc.	Polymorphic crystalline forms of tiacumicin B
CN102614207B (zh) *	2005-01-31	2016-01-13	默克夏普&多梅有限公司	18元环大环化合物及其类似物
ZA200905337B (en)	2007-01-22	2010-10-27	Optimer Pharmaceuticals Inc	Macrocyclic polymorphs, compositions comprising such polymorphs, and methods of use and manufacture thereof
ITMI20120560A1 (it)	2012-04-05	2013-10-06	Olon Spa	Procedimento per la purificazione della tiacumicina b
US8722863B2 (en)	2012-05-10	2014-05-13	Teva Pharmaceutical Works Ltd.	Solid state forms of fidaxomycin and processes for preparation thereof
WO2013170142A1 (fr)	2012-05-10	2013-11-14	Teva Pharmaceutical Works Ltd.	Formes à l'état solide de fidaxomycine et procédés pour la préparation de celles-ci

2015
- 2015-03-17 CA CA2940902A patent/CA2940902C/fr active Active
- 2015-03-17 PT PT157111220T patent/PT3119793T/pt unknown
- 2015-03-17 US US15/126,347 patent/US10227371B2/en active Active
- 2015-03-17 SI SI201530241T patent/SI3119793T1/en unknown
- 2015-03-17 PL PL15711122T patent/PL3119793T3/pl unknown
- 2015-03-17 DK DK15711122.0T patent/DK3119793T3/en active
- 2015-03-17 KR KR1020167027975A patent/KR20160134719A/ko not_active Ceased
- 2015-03-17 HU HUE15711122A patent/HUE038426T2/hu unknown
- 2015-03-17 HR HRP20180668TT patent/HRP20180668T1/hr unknown
- 2015-03-17 ES ES15711122.0T patent/ES2668351T3/es active Active
- 2015-03-17 WO PCT/EP2015/055531 patent/WO2015140153A1/fr not_active Ceased
- 2015-03-17 AU AU2015233583A patent/AU2015233583B2/en active Active
- 2015-03-17 JP JP2016558001A patent/JP2017507994A/ja active Pending
- 2015-03-17 CN CN201580013984.XA patent/CN106103462A/zh active Pending
- 2015-03-17 BR BR112016021542-7A patent/BR112016021542B1/pt active IP Right Grant
- 2015-03-17 EP EP15711122.0A patent/EP3119793B1/fr active Active
2016
- 2016-09-08 IL IL247726A patent/IL247726A0/en unknown
2019
- 2019-03-05 IL IL265180A patent/IL265180B/en unknown

Also Published As

Publication number	Publication date
PL3119793T3 (pl)	2018-07-31
BR112016021542A2 (fr)	2017-08-15
US10227371B2 (en)	2019-03-12
PT3119793T (pt)	2018-05-10
SI3119793T1 (en)	2018-06-29
EP3119793A1 (fr)	2017-01-25
DK3119793T3 (en)	2018-05-22
BR112016021542B1 (pt)	2023-01-31
KR20160134719A (ko)	2016-11-23
AU2015233583B2 (en)	2019-04-11
IL265180B (en)	2022-01-01
US20170081355A1 (en)	2017-03-23
HUE038426T2 (hu)	2018-10-29
CN106103462A (zh)	2016-11-09
WO2015140153A1 (fr)	2015-09-24
IL265180A (en)	2019-05-30
CA2940902C (fr)	2022-10-25
HRP20180668T1 (hr)	2018-06-15
CA2940902A1 (fr)	2015-09-24
EP3119793B1 (fr)	2018-03-14
JP2017507994A (ja)	2017-03-23
IL247726A0 (en)	2016-11-30
AU2015233583A1 (en)	2016-09-15

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